TR200102109T2 - Ras-farnesyltransferase inhibitor and sulfobutylether-7-ß-cyclodextrin or 2-hydroxypropyl-ß-cyclodextrin complex and method. - Google Patents
Ras-farnesyltransferase inhibitor and sulfobutylether-7-ß-cyclodextrin or 2-hydroxypropyl-ß-cyclodextrin complex and method.Info
- Publication number
- TR200102109T2 TR200102109T2 TR2001/02109T TR200102109T TR200102109T2 TR 200102109 T2 TR200102109 T2 TR 200102109T2 TR 2001/02109 T TR2001/02109 T TR 2001/02109T TR 200102109 T TR200102109 T TR 200102109T TR 200102109 T2 TR200102109 T2 TR 200102109T2
- Authority
- TR
- Turkey
- Prior art keywords
- ras
- cyclodextrin
- complex
- sulfobutylether
- hydroxypropyl
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Abstract
Bir ras-farnesiltransferazi inhibitörü kompleksi olup, formül (I)'i havi ras-farnesiltransferazi inhibitörünü veya bunun farmasötik yönden kabul edilebilir bir tuzunu ve sülfobütileter-7- -siklodekstrini veya 2-hidroksipropil- -siklodekstrini ihtiva eder, ve burada n 0 veya 1'dir; R1 C1, Br, fenil, piridil veya siyanodan seçilir; R2 aralkildir; R3 sayica düsük karbonlu alkil, aril, veya ikameli/katkili aril veya heterosiklodan seçilir; Z1 CO, SO2, CO2, SO2NR5 den seçilir ve burada R5 hidrojen, sayica düsük karbonlu alkil veya ikameli/katkili alkilden seçilir. Bu kompleks ras-farnesiltrasferazi inhibitörünün beklenmedik derecede yüksek olan bir suda erime kabiliyetini ortaya koyar ve kansere yakalanmis olan insanlara damar içine uygulanmaya uygundur. Kompleksin meydana getirilmesine yönelik bir metod da ortaya konulmaktadir. Ras-farnesiltransferazi inhibitörleri anti-tümör ajanlar olarak faydalidir.A ras-farnesyltransferase inhibitor complex comprising ras-farnesyltransferase inhibitor of formula (I) and a pharmaceutically acceptable salt thereof and sulfobutylether-7- -cyclodextrin or 2-hydroxypropyl--cyclodextrin where n 0 or 1 'd; R1 is selected from C1, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower-carbon alkyl, aryl, or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2, SO2NR5, where R5 is selected from hydrogen, low-carbon alkyl, or substituted alkyl. This complex demonstrates the unexpectedly high water-solubility of the ras-farnesyltrasferase inhibitor and is suitable for intravenous administration to people with cancer. A method of forming the complex is also disclosed. Ras-farnesyltransferase inhibitors are useful as anti-tumor agents.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11664799P | 1999-01-21 | 1999-01-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TR200102109T2 true TR200102109T2 (en) | 2001-12-21 |
Family
ID=22368422
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TR2001/02109T TR200102109T2 (en) | 1999-01-21 | 1999-12-21 | Ras-farnesyltransferase inhibitor and sulfobutylether-7-ß-cyclodextrin or 2-hydroxypropyl-ß-cyclodextrin complex and method. |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US6218375B1 (en) |
| EP (1) | EP1143796A4 (en) |
| JP (1) | JP2002535253A (en) |
| KR (1) | KR100708360B1 (en) |
| CN (1) | CN1219517C (en) |
| AR (1) | AR022323A1 (en) |
| AU (1) | AU772204B2 (en) |
| BG (1) | BG105666A (en) |
| BR (1) | BR9916566A (en) |
| CA (1) | CA2359646C (en) |
| CO (1) | CO5160253A1 (en) |
| CZ (1) | CZ20012601A3 (en) |
| EE (1) | EE200100382A (en) |
| GE (1) | GEP20043214B (en) |
| HK (1) | HK1038865A1 (en) |
| HU (1) | HUP0105160A3 (en) |
| ID (1) | ID30139A (en) |
| IL (1) | IL144025A (en) |
| LT (1) | LT4893B (en) |
| LV (1) | LV12712B (en) |
| MY (1) | MY119700A (en) |
| NO (1) | NO20013585L (en) |
| NZ (1) | NZ511995A (en) |
| PE (1) | PE20001419A1 (en) |
| PL (1) | PL195280B1 (en) |
| RU (1) | RU2230062C2 (en) |
| SK (1) | SK9602001A3 (en) |
| TR (1) | TR200102109T2 (en) |
| TW (1) | TWI232752B (en) |
| UA (1) | UA67825C2 (en) |
| UY (2) | UY25986A1 (en) |
| WO (1) | WO2000042849A1 (en) |
| ZA (1) | ZA200104416B (en) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI310684B (en) * | 2000-03-27 | 2009-06-11 | Bristol Myers Squibb Co | Synergistic pharmaceutical kits for treating cancer |
| JP2003063965A (en) * | 2001-06-13 | 2003-03-05 | Otsuka Pharmaceut Factory Inc | Cilostazol aqueous composition for injection |
| US6566347B1 (en) * | 2001-08-22 | 2003-05-20 | Duquesne University Of The Holy Ghost | Controlled release pharmaceutical |
| AU2002359412A1 (en) * | 2001-11-13 | 2003-05-26 | Bristol-Myers Squibb Company | Process for the preparation of 3,7-disubstituted-2,3,4,5- tetrahydro-1h-1,4-benzodiazepine compounds |
| KR100451485B1 (en) | 2002-03-28 | 2004-10-06 | 주식회사종근당 | Inclusion compounds of fumagillol derivative or its salt, and pharmaceutical compositions comprising the same |
| US6869939B2 (en) * | 2002-05-04 | 2005-03-22 | Cydex, Inc. | Formulations containing amiodarone and sulfoalkyl ether cyclodextrin |
| WO2003106628A2 (en) * | 2002-06-17 | 2003-12-24 | Bristol-Myers Squibb Company | Benzodiazepine inhibitors of mitochondial f1f0 atp hydrolase and methods of inhibiting f1f0 atp hydrolase |
| US7157446B2 (en) * | 2003-05-02 | 2007-01-02 | Bristol Myers Squibb Company | Complex of ras-farnesyltransferase inhibitor, a cyclodextrin, and ethanol |
| US20070020299A1 (en) | 2003-12-31 | 2007-01-25 | Pipkin James D | Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid |
| US20100204178A1 (en) * | 2006-10-02 | 2010-08-12 | James Cloyd | Novel parenteral carbamazepine formulation |
| EP1928464B1 (en) | 2005-09-30 | 2014-05-14 | Lundbeck Inc. | Novel parenteral carbamazepine formulation |
| CN100503647C (en) * | 2005-11-02 | 2009-06-24 | 南京师范大学 | Hydroxypropyl- sulfobutyl-beta- cyclodextrin and its preparation method, analytical method and pharmaceutical uses |
| TW200806284A (en) * | 2006-03-31 | 2008-02-01 | Alcon Mfg Ltd | Prenyltransferase inhibitors for ocular hypertension control and the treatment of glaucoma |
| KR20090087079A (en) * | 2006-11-21 | 2009-08-14 | 노파르티스 아게 | Stable parenteral formulation containing a rsv inhibitor of a benzodiazepine structure |
| SG10201914059WA (en) | 2008-10-22 | 2020-03-30 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| NZ604498A (en) | 2010-05-26 | 2014-10-31 | Neurophyxia B V | 2-iminobiotin formulations and uses thereof |
| WO2012034038A2 (en) * | 2010-09-09 | 2012-03-15 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Dual inhibitors of farnesyltransferase and geranylgeranyltransferase i |
| US9309203B2 (en) * | 2011-10-07 | 2016-04-12 | Pisces Therapeutics, Llc | Malignant and non-malignant disease treatment with Ras antagonists |
| CN105194685A (en) * | 2015-10-15 | 2015-12-30 | 重庆大学 | Sulphaguanidine and sulfobutyl ether-beta-cyclodextrin inclusion compound and powder injection preparation |
| JP6975165B2 (en) | 2015-12-16 | 2021-12-01 | ニューロフィシア・ベー・フェー | 2-Iminobiotin for use in the treatment of brain cell injury |
| PE20181888A1 (en) | 2016-04-04 | 2018-12-11 | Loxo Oncology Inc | LIQUID FORMULATIONS OF (S) -N- (5 - ((R) -2- (2,5-DIFLUOROPHENYL) -PYRROLIDIN-1-IL) -PYRAZOLE [1,5-A] PYRIMIDIN-3-IL) -3 -HYDROXYPYRROLIDINE-1-CARBOXAMIDE |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| RU2745953C2 (en) | 2016-05-18 | 2021-04-05 | Локсо Онколоджи, Инк. | Method for making (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrolidine-1-carboxamide and its salts |
| JOP20190092A1 (en) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF |
| US20210145816A1 (en) * | 2019-11-15 | 2021-05-20 | Cyclolab Cyclodextrin Research And Development Laboratory Ltd. | Pharmaceutical formulation of lonafarnib with a sulfobutylether beta-cyclodextrin |
| WO2023113479A1 (en) * | 2021-12-15 | 2023-06-22 | Sillajen, Inc. | Pharmaceutical compositions comprising modified beta-cyclodextrins |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5630927A (en) * | 1979-08-24 | 1981-03-28 | Zeria Shinyaku Kogyo Kk | Stabilization of guaiazulene and its derivative |
| US4371673A (en) * | 1980-07-21 | 1983-02-01 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Water soluble forms of retinoids |
| US4727064A (en) * | 1984-04-25 | 1988-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Pharmaceutical preparations containing cyclodextrin derivatives |
| US4596795A (en) * | 1984-04-25 | 1986-06-24 | The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services | Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives |
| KR0166088B1 (en) * | 1990-01-23 | 1999-01-15 | . | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| JPH07165616A (en) * | 1993-12-09 | 1995-06-27 | Hisamitsu Pharmaceut Co Inc | Complex composition of cyclodextrin and method for making complex |
| US6011029A (en) * | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
| JPH1067639A (en) * | 1996-08-26 | 1998-03-10 | Shiseido Co Ltd | Vitamin e-vitamin c phosphoric diester/cyclodextrin clathrate and external preparation for skin containing the same |
-
1999
- 1999-12-21 EP EP99967470A patent/EP1143796A4/en not_active Withdrawn
- 1999-12-21 AU AU23740/00A patent/AU772204B2/en not_active Ceased
- 1999-12-21 NZ NZ511995A patent/NZ511995A/en unknown
- 1999-12-21 RU RU2001118265/04A patent/RU2230062C2/en not_active IP Right Cessation
- 1999-12-21 HU HU0105160A patent/HUP0105160A3/en unknown
- 1999-12-21 ID IDW00200101596A patent/ID30139A/en unknown
- 1999-12-21 KR KR1020017009131A patent/KR100708360B1/en not_active IP Right Cessation
- 1999-12-21 SK SK960-2001A patent/SK9602001A3/en unknown
- 1999-12-21 GE GEAP19995955A patent/GEP20043214B/en unknown
- 1999-12-21 TR TR2001/02109T patent/TR200102109T2/en unknown
- 1999-12-21 JP JP2000594323A patent/JP2002535253A/en active Pending
- 1999-12-21 EE EEP200100382A patent/EE200100382A/en unknown
- 1999-12-21 WO PCT/US1999/030424 patent/WO2000042849A1/en active IP Right Grant
- 1999-12-21 CN CNB998157074A patent/CN1219517C/en not_active Expired - Fee Related
- 1999-12-21 PL PL99366338A patent/PL195280B1/en not_active IP Right Cessation
- 1999-12-21 CZ CZ20012601A patent/CZ20012601A3/en unknown
- 1999-12-21 BR BR9916566-0A patent/BR9916566A/en not_active Application Discontinuation
- 1999-12-21 CA CA002359646A patent/CA2359646C/en not_active Expired - Fee Related
- 1999-12-21 IL IL14402599A patent/IL144025A/en not_active IP Right Cessation
- 1999-12-21 UA UA2001085843A patent/UA67825C2/en unknown
- 1999-12-31 MY MYPI99005834A patent/MY119700A/en unknown
-
2000
- 2000-01-14 TW TW089100557A patent/TWI232752B/en not_active IP Right Cessation
- 2000-01-17 US US09/483,840 patent/US6218375B1/en not_active Expired - Lifetime
- 2000-01-18 CO CO00002434A patent/CO5160253A1/en unknown
- 2000-01-20 AR ARP000100255A patent/AR022323A1/en unknown
- 2000-01-21 PE PE2000000046A patent/PE20001419A1/en not_active Application Discontinuation
- 2000-01-21 UY UY25986A patent/UY25986A1/en unknown
- 2000-01-21 UY UY25987A patent/UY25987A1/en not_active Application Discontinuation
-
2001
- 2001-05-29 ZA ZA200104416A patent/ZA200104416B/en unknown
- 2001-06-21 LT LT2001064A patent/LT4893B/en not_active IP Right Cessation
- 2001-07-03 BG BG105666A patent/BG105666A/en unknown
- 2001-07-04 LV LVP-01-101A patent/LV12712B/en unknown
- 2001-07-20 NO NO20013585A patent/NO20013585L/en not_active Application Discontinuation
-
2002
- 2002-01-08 HK HK02100115.8A patent/HK1038865A1/en unknown
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